Idraparinux
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Routes of administration | Subcutaneous |
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Pharmacokinetic data | |
Elimination half-life | 80-130 hours |
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Idraparinux sodium is an
It has a similar chemical structure and the same method of action as fondaparinux, but with an elimination half-life about five to six times longer (an increase from fondaparinux's 17 hours to approximately 80 hours), which means that the drug should only need to be injected once a week. Supriya Dey et al recently reported shortest chemical synthesis of Idraparinux for the large-scale production.[citation needed]
Sanofi discontinued the development of idraparinux sodium.
Negative clinical trial
A phase III trial of idraparinux sodium for stroke prevention in patients with AF (AMADEUS) was halted prematurely due to excessive clinically relevant and intracranial bleeding. Bleedings were particularly increased in elderly patients and those with renal impairment. Sanofi discontinued the development of idraparinux sodium in favour of a biotinylated formulation of the drug called idrabiotaparinux sodium.[2][3]
Method of action
Idraparinux selectively blocks
See Heparin: Mechanism of anticoagulant action for a comparison of the mechanism of heparin, low-molecular-weight heparins, fondaparinux and idraparinux.
Idrabiotaparinux
Idrabiotaparinux sodium is also administered once-weekly. It has the same pentasaccharidic structure as idraparinux sodium, but with biotin attached, which allows its neutralisation with avidin, an egg-derived protein with low antigenicity. Sanofi conducted three phase III trials of idrabiotaparinux sodium between 2006 and 2008 in approximately 13,550 patients. In one phase III trial (the BOREALIS-AF study), idrabiotaparinux sodium was non-inferior to warfarin in preventing the recurrent
References
- S2CID 37919.
- ^ Modern anticoagulants threaten status quo http://www.pmlive.com/pharma_intelligence/modern_anticoagulants_threaten_status_quo_411610
- ^ The Amadeus investigators. Comparison of idraparinux with vitamin K antagonists for prevention of thromboembolism in patients with atrial fibrillation: a randomised, open-label, non-inferiority trial. Lancet 2008; 371:315-321.
- PMID 17855670.
- ^ Stroke Prevention in Atrial Fibrillation: Latest Clinical Trials and Guidelines Luciana Armaganijan, Dimpi Patel, [...], and Carlos A. Morillo Pharmaceuticals (Basel). Apr 2012; 5(4): 384–397 doi: 10.3390/ph5040384
- ^ Modern anticoagulants threaten status quo http://www.pmlive.com/pharma_intelligence/modern_anticoagulants_threaten_status_quo_411610
- ^ Song Y, Li X, Pavithra S, Li D (2013) Idraparinux or Idrabiotaparinux for Long-Term Venous Thromboembolism Treatment: A Systematic Review and Meta-Analysis of Randomized Controlled Trials. PLoS ONE 8(11): e78972. doi:10.1371/journal.pone.0078972
8. Supriya Dey, Hong Jay Lo and Chi Huey Wong “ An efficient Modular One pot synthesis of Heparin-Based Anticoagulant Idraparinux” J. Am. Chem. Soc. 2019, 141, 10309